Inhibitors of protein isoprenyl transferases

US6693123B2 · kind B2 · utility

Assignee

• UNIVERSITY OF PITTSBURGH · US

Inventors

• Said M. Sebti · Tampa, US
• Andrew D. Hamilton · Felton, GB
• David J. Augeri · Princeton, US
• Kenneth J. Barr · San Francisco, US
• Greg B. Donner · Mundelein, US
• Stephen A. Fakhoury · Mundelein, US
• Stephen O'Connor · Wilmette, US
• Saul H. Rosenberg · Grayslake, US
• Wang Shen · San Mateo, US
• Bruce Szczepankiewicz · Gages Lake, US
• Indrani W. Gunawardana · Boulder, US

Key dates

• Filing date: Oct 30, 2001
• Grant date: Feb 17, 2004
• Expiry date: Mar 1, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2603/74
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5—, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting com…